Antinociceptive and antitumor activity of novel synthetic mononuclear ruthenium (II) compounds

Shyam Sunder Anchuri, Satyavathi Dhulipala, Sreekanth Thota, Rajeshwar Yerra, Jan Balzarini, Erik D. Clercq


  • Background: From the thousands of years, metal compounds have been used in medicine for treatment of various diseases including various types of cancers. Ruthenium was seen as a promising metal due to its similar kinetics to platinum and its lower toxicity. Therefore, we aimed to evaluate the newer mononuclear ruthenium (II) compounds for antinociceptive and antitumor activities.
  • Materials and Methods: Ruthenium (II) compounds were evaluated for antinociceptive and antitumor activity using the various in vitro and in vivo models. The compounds were injected to mice at concentrations of 1 and 2 mg kg-1 intraperitoneally and were screened for antinociceptive activity, and the antiproliferative effect was evaluated against murine leukemia cells (L1210), human T-lymphocyte cells (CEM) and human cervix carcinoma cells (HeLa) using MTT assay.
  • Results: The results for antitumor activity clearly indicated that compound R1 was potent cytotoxic agent than R2 with IC50 values ranging from 4-6 µM for R1, whereas IC50 values for compound R2 ranging from 65-103 µM. The compounds have shown a significant anti-inflammatory effect in carrageenan and dextran models but do not having the central analgesic activity, this indicating that the antinociceptive activity is related to the peripheral nervous system. The results for 5-Lipoxygenase (5-LOX) activity showed that both R1and R2 compounds were found to be significant 5-LOX inhibitory activity with IC50 values of 14.35 µ and 29.24 µ respectively.
  • Conclusion: These findings concluded that the new ruthenium compounds might be the promising antiproliferative agents as these compounds showing significant 5-LOX inhibitory activity and potential agents in the management of pain related disorders.
  • Keywords: 5-LOX, antinociception, MTT, ruthenium compounds

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